The pharmacological profile of the competitive muscarinic antagonist S-(-)-o- (hydroxymethyl)benzeneacetic acid I-methyl-4-piperidinyl ester (S-(-)-ET 126) was evaluated on Ml (rabbit vas deferens; pA2=8.99), M2 (rat left atrium; pA2=8.21) and M3 (rat ileum; pA2=6.84) muscarinic receptors in comparison with pirenzepine. The drug shows a subtype selectivity (Ml/Mz=8; Mt/M3=178; M2/M3=22) that proposes it as a useful pharmacological tool for receptor studies. S-(-)-ET 126, like pirenzepine, prevents the antinociception induced by Mt agonists (McN-A-343 and AF-102B). Unlike pirenzepine and spirotramine, the compound is able to cross the blood brain barrier which makes it useful for in vivo investigations.
S(-)ET126: a potent and selective M1 antagonist in vitro and in vivo / C. GHELARDINI; A. BARTOLINI; N. GALEOTTI; E. TEODORI; F. GUALTIERI. - In: LIFE SCIENCES. - ISSN 0024-3205. - STAMPA. - 58:(1996), pp. 991-1000. [10.1016/0024-3205(96)00047-1]
S(-)ET126: a potent and selective M1 antagonist in vitro and in vivo
GHELARDINI, CARLA;BARTOLINI, ALESSANDRO;GALEOTTI, NICOLETTA;TEODORI, ELISABETTA;GUALTIERI, FULVIO
1996
Abstract
The pharmacological profile of the competitive muscarinic antagonist S-(-)-o- (hydroxymethyl)benzeneacetic acid I-methyl-4-piperidinyl ester (S-(-)-ET 126) was evaluated on Ml (rabbit vas deferens; pA2=8.99), M2 (rat left atrium; pA2=8.21) and M3 (rat ileum; pA2=6.84) muscarinic receptors in comparison with pirenzepine. The drug shows a subtype selectivity (Ml/Mz=8; Mt/M3=178; M2/M3=22) that proposes it as a useful pharmacological tool for receptor studies. S-(-)-ET 126, like pirenzepine, prevents the antinociception induced by Mt agonists (McN-A-343 and AF-102B). Unlike pirenzepine and spirotramine, the compound is able to cross the blood brain barrier which makes it useful for in vivo investigations.
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